Porfimer sodium

Identification

Summary

Porfimer sodium is a hematoporphyrin derivative used to treat esophageal cancer, endobronchial cancer, and high grade dysplasia in Barrett's Esophagus.

Brand Names
Photofrin
Generic Name
Porfimer sodium
DrugBank Accession Number
DB00707
Background

The purified component of hematoporphyrin derivative, it consists of a mixture of oligomeric porphyrins. It is used in photodynamic therapy (hematoporphyrin photoradiation); to treat malignant lesions with visible light and experimentally as an antiviral agent. It is the first drug to be approved in the use of photodynamic therapy in the United States.

Type
Small Molecule
Groups
Approved, Investigational
Synonyms
  • Porfimer natrium
  • Porfimer sodico
  • Porfimer sodium
  • Porfimère sodique
  • Porfimerum natricum

Pharmacology

Indication

Indicated in the treatment of esophageal cancer.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Porfimer is a photosensitizing agent used in the photodynamic therapy (PDT) of tumors. Porfimer is indicated for the palliation of patients with completely obstructing esophageal cancer, or of patients with partially obstructing esophageal cancer who cannot be satisfactorily treated with Nd:YAG laser therapy, reduction of obstruction and palliation of symptoms in patients with completely or partially obstructing endobronchial nonsmall cell lung cancer (NSCLC), and the treatment of microinvasive endobronchial NSCLC in patients for whom surgery and radiotherapy are not indicated. The cytotoxic and antitumor actions of porfimer are light and oxygen dependent. Tumor selectivity in treatment occurs through a combination of selective retention of porfimer and selective delivery of light.

Mechanism of action

Cellular damage caused by porfimer is a consequence of the propagation of radical reactions. Radical initiation may occur after porfimer absorbs light to form a porphyrin excited state. Spin transfer from porfimer to molecular oxygen may then generate singlet oxygen. Subsequent radical reactions can form superoxide and hydroxyl radicals. Tumor death also occurs through ischemic necrosis secondary to vascular occlusion that appears to be partly mediated by thromboxane A2 release.

TargetActionsOrganism
ULow-density lipoprotein receptor
other/unknown
Humans
UHigh affinity immunoglobulin gamma Fc receptor I
antagonist
Humans
Absorption

Not Available

Volume of distribution
  • 0.49 ± 0.28 L/kg [2 mg/kg dose of porfimer sodium to 4 male cancer patients]
Protein binding

~90%

Metabolism
Not Available
Route of elimination

Not Available

Half-life

10-452 hours

Clearance
  • Renal cl=199.7 +/-  56.9 mL/min [Healthy subjects receiving a single 300-mg oral dose]
Adverse Effects
Adverseeffects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
Aminolevulinic acidAminolevulinic acid may increase the photosensitizing activities of Porfimer sodium.
CarprofenCarprofen may increase the photosensitizing activities of Porfimer sodium.
ClofazimineClofazimine may increase the photosensitizing activities of Porfimer sodium.
CyproheptadineCyproheptadine may increase the photosensitizing activities of Porfimer sodium.
DabrafenibDabrafenib may increase the photosensitizing activities of Porfimer sodium.
Darbepoetin alfaThe risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Porfimer sodium.
ErythropoietinThe risk or severity of Thrombosis can be increased when Erythropoietin is combined with Porfimer sodium.
FebuxostatFebuxostat may increase the photosensitizing activities of Porfimer sodium.
FosdenopterinFosdenopterin may increase the photosensitizing activities of Porfimer sodium.
HexaminolevulinateHexaminolevulinate may increase the photosensitizing activities of Porfimer sodium.
Interactions
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Food Interactions
No interactions found.

Products

Products2
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International/Other Brands
PhotoBarr (Axcan) / Photofrin II
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
PhotofrinInjection, powder, for solution2.5 mg/1mLIntravenousAxcan Scandipharm Inc.2006-09-11Not applicableUS flag
PhotofrinPowder, for solution15 mg / vialIntravenousConcordia Pharmaceuticals, Inc1995-12-312014-11-21Canada flag
PhotofrinInjection, powder, for solution75 mg/31.8mLIntravenousPinnacle Biologics, Inc.1995-12-27Not applicableUS flag
PhotofrinPowder, for solution75 mg / vialIntravenousConcordia Pharmaceuticals, Inc1995-12-312019-07-18Canada flag

Categories

ATC Codes
L01XD01 — Porfimer sodium
Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
Y3834SIK5F
CAS number
87806-31-3

References

General References
Not Available
PubChem Substance
46508600
ChemSpider
10482043
RxNav
333848
ChEBI
60652
PharmGKB
PA164752658
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Porfimer_sodium
FDA label
Download (321 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentBrain and Central Nervous System Tumors1
3CompletedTreatmentCancer of the Gallbladder / Extrahepatic Bile Duct Cancer1
3TerminatedTreatmentHilar Cholangiocarcinoma1
3Unknown StatusTreatmentBrain and Central Nervous System Tumors1
3Unknown StatusTreatmentStage I Esophageal Adenocarcinoma / Stage I Esophageal Squamous Cell Carcinoma / Stage II Esophageal Adenocarcinoma / Stage II Esophageal Squamous Cell Carcinoma / Stage III Oesophageal Adenocarcinoma / Stage III Oesophageal squamous cell carcinoma1
3WithdrawnTreatmentCholangiocarcinoma of the Extrahepatic Bile Duct / Cholangiocarcinoma of the Gallbladder / Recurrent Extrahepatic Bile Duct Cancer / Recurrent Gallbladder Cancer / Unresectable Extrahepatic Bile Duct Cancer / Unresectable Gallbladder Cancer1
2CompletedDiagnosticHead and Neck Carcinoma1
2CompletedTreatmentCancer of the Gallbladder / Extrahepatic Bile Duct Cancer / Liver Cancer / Malignant Neoplasm of Pancreas1
2CompletedTreatmentEsophageal Neoplasms Malignant1
2CompletedTreatmentHead and Neck Carcinoma / Precancerous/Nonmalignant Condition1

Pharmacoeconomics

Manufacturers
  • Axcan pharma us inc
Packagers
  • Axcan Pharma Inc.
  • Draxis Specialty Pharmaceuticals Inc.
Dosage Forms
FormRouteStrength
Injection, powder, for solutionIntravenous2.5 mg/1mL
Injection, powder, for solutionIntravenous75 mg/31.8mL
Powder, for solutionIntravenous
Powder, for solutionIntravenous15 mg / vial
Powder, for solutionIntravenous75 mg / vial
Prices
Unit descriptionCostUnit
Photofrin 75 mg vial3317.04USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5145863No1992-09-082009-12-15US flag
CA2094974No1996-10-222013-04-27Canada flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP2.8Not Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Other/unknown
General Function
Virus receptor activity
Specific Function
Binds LDL, the major cholesterol-carrying lipoprotein of plasma, and transports it into cells by endocytosis. In order to be internalized, the receptor-ligand complexes must first cluster into clat...
Gene Name
LDLR
Uniprot ID
P01130
Uniprot Name
Low-density lipoprotein receptor
Molecular Weight
95375.105 Da
References
  1. Korbelik M: Low density lipoprotein receptor pathway in the delivery of Photofrin: how much is it relevant for selective accumulation of the photosensitizer in tumors? J Photochem Photobiol B. 1992 Jan;12(1):107-9. [Article]
  2. Tsukagoshi S: [Porfimer sodium (Photofrin-II)]. Gan To Kagaku Ryoho. 1995 Aug;22(9):1271-8. [Article]
  3. Maziere JC, Mora L, Biade S, Maziere C, Santus R: [Potentiation of the photocytotoxic effect of photofrin II: synergistic action of verapamil and lovastatin]. Bull Acad Natl Med. 1994 Jun;178(6):1177-88; discussion 1188-9. [Article]
  4. Candide C, Morliere P, Maziere JC, Goldstein S, Santus R, Dubertret L, Reyftmann JP, Polonovski J: In vitro interaction of the photoactive anticancer porphyrin derivative photofrin II with low density lipoprotein, and its delivery to cultured human fibroblasts. FEBS Lett. 1986 Oct 20;207(1):133-8. [Article]
  5. Maziere JC, Morliere P, Biade S, Santus R: [Antitumor photochemotherapy: biochemical bases, therapeutic uses and perspectives]. C R Seances Soc Biol Fil. 1992;186(1-2):88-106. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Receptor signaling protein activity
Specific Function
High affinity receptor for the Fc region of immunoglobulins gamma. Functions in both innate and adaptive immune responses.
Gene Name
FCGR1A
Uniprot ID
P12314
Uniprot Name
High affinity immunoglobulin gamma Fc receptor I
Molecular Weight
42631.525 Da
References
  1. Krutmann J, Athar M, Mendel DB, Khan IU, Guyre PM, Mukhtar H, Elmets CA: Inhibition of the high affinity Fc receptor (Fc gamma RI) on human monocytes by porphyrin photosensitization is highly specific and mediated by the generation of superoxide radicals. J Biol Chem. 1989 Jul 5;264(19):11407-13. [Article]

Drug created on June 13, 2005 13:24 / Updated on October 19, 2021 07:39